Topotecan Hydrochloride (SKF 104864A; NSC 609669) is a Topoisomerase I inhibitor with potent antineoplastic activities.
2'-Deoxyadenosine-5'-triphosphate-d14 (dATP-d14) dilithium is deuterium labeled 2'-Deoxyadenosine-5'-triphosphate (HY-136648). 2'-Deoxyadenosine-5'-triphosphate (dATP) is a nucleotide used in cells for DNA synthesis (or replication), as a substrate of DNA polymerase.
LMP744 hydrochloride (MJ-III65 hydrochloride) is a DNA intercalator and Topoisomerase (Top1) inhibitor with antitumor activity[1].
5'-O-DMT-ibu-dC can be used in the synthesis of oligodeoxyribonucleotides[1].
4,5,6,7-Tetrabromobenzimidazole is a selective and ATP competitive CK2 (casein kinase 2) inhibitor[1].
NU1025 is a potent PARP inhibitor with an IC50 of 400 nM and a Ki of 48 nM. NU1025 potentiates the cytotoxicity of ionizing radiation and anticancer drugs. NU1025 has anti-cancer and neuroprotective activity[1][2][3].
Hydroxyurea is a cell apoptosis inducer that inhibitDNA synthesis through inhibition of ribonucleotide reductase.
2-Chloro-6-(furan-2-yl) purine-beta-D-(3’-deoxy-3’-fluoro)-riboside is a purine nucleoside analogue. Purine nucleoside analogs have broad antitumor activity targeting indolent lymphoid malignancies. Anticancer mechanisms in this process rely on inhibition of DNA synthesis, induction of apoptosis, etc[1].
Palbociclib D8 (PD 0332991 D8) is a deuterium labeled Palbociclib. Palbociclib is a selective and orally active CDK4 and CDK6 inhibitor with IC50s of 11 and 16 nM, respectively. Palbociclib has no activity against other protein kinases. Palbociclib has potently anticancer activities[1].
Chlamydocin, a fungal metabolite, is a highly potent HDAC inhibitor, with an IC50 of 1.3 nM. Chlamydocin exhibits potent antiproliferative and anticancer activities. Chlamydocin induces apoptosis by activating caspase-3[1].
5-(N-Isopentenyl-N-trifluoroacetyl) aminomethyluridine is a purine nucleoside analogue. Purine nucleoside analogs have broad antitumor activity targeting indolent lymphoid malignancies. Anticancer mechanisms in this process rely on inhibition of DNA synthesis, induction of apoptosis, etc[1].
BRCA1-IN-2 (compound 15) is a cell-permeable protein-protein interaction (PPI) inhibitor for BRCA1 with an IC50 of 0.31 μM and a Kd of 0.3 μM, which shows antitumor activities via the disruption of BRCA1 (BRCT)2/protein interactions[1].
Dehydroaltenusin is a small molecule selective inhibitor of eukaryotic DNA polymerase α, a type of antibiotic produced by a fungus with an IC50 value of 0.68 μM. The inhibitory mode of action of dehydroaltenusin against mammalian pol α activity is competitive with respect to the DNA template primer (Ki=0.23 µM) and non-competitive with respect to the 2'-deoxyribonucleoside 5'-triphosphate substrate (Ki=0.18 µM)[1].Dehydroaltenusin arrests the cancer cell cycle at the S-phase and triggers apoptosis[1].Dehydroaltenusin possesses anti-tumor activity against human adenocarcinoma tumor in vivo[1].
7-Allyl-7,8-dihydro-8-oxo-9-(β-D-xylofuranosyl) guanine is a purine nucleoside analogue. Purine nucleoside analogs have broad antitumor activity targeting indolent lymphoid malignancies. Anticancer mechanisms in this process rely on inhibition of DNA synthesis, induction of apoptosis, etc[1].
PBOX 6 is a pyrrolo-1,5-benzoxazepine (PBOX) compound, acts as a microtubule-depolymerizing agent and an apoptotic agent.
5’-O-DMTr-3’-deoxyuridine 2’-CED phosphoramidite is a purine nucleoside analog. Purine nucleoside analogs have broad antitumor activity targeting indolent lymphoid malignancies. Anticancer mechanisms in this process rely on inhibition of DNA synthesis, induction of apoptosis, etc[1].
Tetrapeptide, an analogue of α-MSH, induces melanin synthesis. Tetrapeptide diminishes DNA damage by reducing the production of reactive oxidative species and enhancing repair of DNA photoproducts[1].
HDAC-IN-36 (compound 23 g) is an orally active and potent HDAC (histone deacetylase) inhibitor, with an IC50 of 11.68 nM (HDAC6). HDAC-IN-36 promotes apoptosis, autophagy and suppresses migration. HDAC-IN-36 shows anti-tumor and anti-metastatic activity, and can be used for breast cancer research[1].
YKL-5-124 is a novel potent, selective, and covalent CDK7 inhibitor (IC50=53.5 nM), inhibits CDK7/CycH/MAT1 enzymatic activity with IC50 of 9.7 nM; displays biochemical and cellular selectivity for CDK7 over structurally related kinases CDK12/13, and no significant activity against CDK2 and CDK9 (IC50>1 uM); targets and forms a covalent bond with CDK7- cysteine 312 (C312); inhibition of CDK7 by YKL-5-124 elicits a transcriptional signature distinct from that of THZ1, shows no discernible effect on RNA Pol II CTD phosphorylation; recapitulate THZ1-mediated effects on gene expression and CTD phosphorylation when combined with CDK12/13 inhibitor THZ531.
5-Hydroxymethyl-2’-O-(2-methoxyethyl)uridine is a purine nucleoside analogue. Purine nucleoside analogs have broad antitumor activity targeting indolent lymphoid malignancies. Anticancer mechanisms in this process rely on inhibition of DNA synthesis, induction of apoptosis, etc[1].
Duocarmycin analog-2 is a potent DNA alkylating agent. Duocarmycin analog-2 can be used of synthetic immunoconjugate. Duocarmycin analog-2 has antitumor activity[1].
Miriplatin is a chemotherapy agent which belongs to the class of alkylating agents.
7-epi-Taxol is an active metabolite of taxol, with activity comparable to that of taxol against cell replication, promoting microtubule bundle formation and against microtubule depolymerization.
Isochamaejasmin is a biflavonoid with anti-cancer, antiplasmodial and insecticidal activities. Isochamaejasmin displays a potent NF-κB (NF-κB) activation activity. Isochamaejasmin could cause DNA damage and induce Apoptosis via the mitochondrial pathway in AW1 cells[1][2]. Isochamaejasmin also has a moderate antiplasmodial activity (IC50 of 7.3 μM for P. falciparum) and relatively low cytotoxicity (CC50 of 29.0 μM)[3].
7’-OH-N-trityl morpholinothymine (PMO Thymidine Precusor) is a purine nucleoside analog. Purine nucleoside analogs have broad antitumor activity targeting indolent lymphoid malignancies. Anticancer mechanisms in this process rely on inhibition of DNA synthesis, induction of apoptosis, etc[1].
MMV688845 is a nontuberculous mycobacteria (NTM) RNA polymerase inhibitor with bactericidal activity against Mycobacterium abscessus and anti-tuberculosis efficacy[1].
FK614 is an orally active, potent, selective PPARγ modulator (SPPARM). FK614 has different effects on the activation of PPARγ at each stage of adipocyte differentiation. FK614 is a nonthiazolidinedione insulin sensitizer. FK614 can be used for the research of hyperglycemia, hypertriglyceridemia, glucose intolerance and type 2 diabetes[1][2][3].
MSC2504877 (MSC-2504877) a novel small molecule selective tankyrase inhibitor with IC50 of 0.7/0.8 nM against TNKS1/2, shows 771-fold selectivity for TNKS1 over PARP1 (IC50=0.54 uM); increased AXIN2 protein levels and decreased β-catenin levels in APC mutant COLO320DM colorectal tumour cells, suppressed canonical Wnt signalling in SW480 cell line, inhibits the growth of APC mutant colorectal tumour cells; enhances G1 cell cycle arrest and cellular senescence in tumour cells when combined with CDK4/6 inhibitor Palbociclib, suppresses the upregulation of Cyclin D2 and Cyclin E2 caused by palbociclib and enhances the suppression of pRb; Palbociclib plus MSC2504877 combination suppresses hyperproliferation in Apc defective cells in vivo.
Hesperadin is an ATP-competitive inhibitor of aurora B kinase with an IC50 of 250 nM.
Longdaysin is a CK1α, CK1δ, and extracellular signal-regulated kinase 2 (ERK2) inhibitor with IC50s of 5.6 µM, 8.8 µM, and 52 µM, respectively[1][2].